2-fluoro-5-piperidin-4-ylpyridine hydrochloride | 1137950-30-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 英文名称: 2-fluoro-5-piperidin-4-ylpyridine hydrochloride
• 英文别名: 2-Fluoro-5-(piperidin-4-yl)pyridine hydrochloride；2-fluoro-5-piperidin-4-ylpyridine;hydrochloride
• CAS: 1137950-30-1
• 化学式: C₁₀H₁₃FN₂*ClH
• 分子量: 216.686
• InChiKey: FVGXHLPORGIWDG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.11
• 重原子数：
  14
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  24.9
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  (Z)-(3,4-difluorophenyl)[5-(hydroxymethyl)-2-pyridinyl]methanone O-(2-hydroxy-2-methylpropyl)oxime 、 2-fluoro-5-piperidin-4-ylpyridine hydrochloride 以to give the title compound (845 mg) as a white solid的产率得到1-(3,4-Difluorophenyl)-1-(5-{[4-(6-fluoropyridin-3-yl)piperidin-1-yl]methyl}pyridin-2-yl)methanamine dihydrochloride
  参考文献：
  名称：

  DIARYLMETHYLAMIDE DERIVATIVE HAVING MELANIN-CONCENTRATING HORMONE RECEPTOR ANTAGONISM

  摘要：

  [问题] 提供一种黑色素浓缩激素受体拮抗剂，用作中枢疾病、循环系统疾病和代谢疾病的药物。 [解决方法] 提供了一种日萘基甲酰胺衍生物，其表示为式（I）：其中，R1a、R1b、R2a、R2b、R3a和R3b独立地表示氢原子或类似物，R4表示氢原子、C1-6烷基或类似物，R5表示氢原子或类似物，Z表示C1-6烷基或类似物，或者R4和Z共同形成一个含有氮的4-6元杂环，Y1表示H或类似物，Y2表示H，或者Y1和Y2共同形成-O-CH2-，W表示C、SO或类似物，Ar1表示6元芳基或类似物，Ar2表示6元芳基或类似物，环A表示苯环、吡啶环或类似物。

  公开号：

  US20110015198A1

文献信息

• DIARYLMETHYLAMIDE DERIVATIVE HAVING ANTAGONISTIC ACTIVITY ON MELANIN-CONCENTRATING HORMONE RECEPTOR
  申请人：Banyu Pharmaceutical Co., Ltd.

  公开号：EP2272841A1

  公开（公告）日：2011-01-12

  [Problem] To provide a melanin-concentrating hormone receptor antagonist useful as a pharmaceutical agent for central diseases, circulatory diseases, and metabolic diseases. [Means for Resolution] Provided is a diarylmethylamide derivative represented by formula (I): Wherein R1a, R1b, R2a, R2b, R3a, and R3b independently represent a hydrogen atom or the like, R4 represents a hydrogen atom, C1-6 alkyl, or the like, R5 represents a hydrogen atom or the like, Z represents C1-6 alkyl or the like, or R4 and Z together form a 4- to 6-membered nitrogen-containing hetero ring, Y1 represents H or the like, Y2 represents H, or Y1 and Y2 together form - O-CH2-, W represents C, SO, or the like, Ar1 represents 6-membered aryl or the like, Ar2 represents 6-membered aryl or the like, and ring A represents a benzene ring, a pyridine ring, or the like.

  [问题] 提供一种对黑色素浓缩激素受体拮抗剂，用作中枢疾病、循环疾病和代谢疾病的药用制剂。 [解决方法] 提供一种由式(I)表示的二芳基甲酰胺衍生物： 其中R1a、R1b、R2a、R2b、R3a和R3b独立地表示氢原子或类似物，R4表示氢原子、C1-6烷基或类似物，R5表示氢原子或类似物，Z表示C1-6烷基或类似物，或者R4和Z一起形成一个含氮杂环的4-至6-成员环，Y1表示H或类似物，Y2表示H，或者Y1和Y2一起形成-O-CH2-，W表示C、SO或类似物，Ar1表示6-成员芳基或类似物，Ar2表示6-成员芳基或类似物，环A表示苯环、吡啶环或类似物。
• DIARYL KETIMINE DERIVATIVE HAVING ANTAGONISM AGAINST MELANIN-CONCENTRATING HORMONE RECEPTOR
  申请人：Ando Makoto

  公开号：US20100324049A1

  公开（公告）日：2010-12-23

  [Problems] To provide an antagonist of a melanin-concentrating hormone receptor, which is useful as a medicine for a central nervous system disease, a cardiovascular disease or a metabolic disease. [Means for Solving Problems] The antagonist comprises, as an active ingredient, a compound represented by the formula (I) wherein R 1a and R 1b independently represent a hydrogen atom or a C 1-6 alkyl group; R 2a , R 2b , R 3a and R 3b independently represent a hydrogen atom, a C 1-6 alkyl group, or the like; Y represents H or —OH; Z represents —OR 8 , or the like; R 8 represents a hydrogen atom, a C 1-6 alkyl group which may have a substituent, or the like; R 9a and R 9b independently represent a hydrogen atom, a C 1-6 alkyl group, or the like; Ar 1 represents an aromatic carbon ring group, or an aromatic heteroring group; Ar 2 represents a group produced by removing two hydrogen atoms from an aromatic carbon ring, or the like; and the ring group A represents an unsaturated heteroring group.

  [问题] 提供一种黑素浓集激素受体的拮抗剂，该拮抗剂作为治疗中枢神经系统疾病、心血管疾病或代谢疾病的药物是有用的。 [解决问题的手段] 该拮抗剂包含作为活性成分的以下公式（I）所示的化合物： 其中 R1a 和 R1b 分别独立代表一个氢原子或一个C1-6烷基团；R2a、R2b、R3a 和 R3b 分别独立代表一个氢原子、一个C1-6烷基团或类似物；Y代表H或—OH；Z代表—OR8，或类似物；R8代表一个氢原子、一个可能含有取代基的C1-6烷基团或类似物；R9a和R9b分别独立代表一个氢原子、一个C1-6烷基团或类似物；Ar1代表一个芳香碳环族或芳香杂环族；Ar2代表通过从一个芳香碳环中移除两个氢原子而得到的族或类似物；而环族A代表一个不饱和杂环族。
• DIARYLMETHYLAMIDE DERIVATIVE HAVING MELANIN-CONCENTRATING HORMONE RECEPTOR ANTAGONISM
  申请人：Kamijo Kaori

  公开号：US20110015198A1

  公开（公告）日：2011-01-20

  [Problem] To provide a melanin-concentrating hormone receptor antagonist useful as a pharmaceutical agent for central diseases, circulatory diseases, and metabolic diseases. [Means for Resolution] Provided is a diarylmethylamide derivative represented by formula (I): Wherein R 1a , R 1b , R 2a , R 2b , R 3a , and R 3b independently represent a hydrogen atom or the like, R 4 represents a hydrogen atom, C 1-6 alkyl, or the like, R 5 represents a hydrogen atom or the like, Z represents C 1-6 alkyl or the like, or R 4 and Z together form a 4- to 6-membered nitrogen-containing hetero ring, Y 1 represents H or the like, Y 2 represents H, or Y 1 and Y 2 together form —O—CH 2 —, W represents C, SO, or the like, Ar 1 represents 6-membered aryl or the like, Ar 2 represents 6-membered aryl or the like, and ring A represents a benzene ring, a pyridine ring, or the like.

  [问题] 提供一种黑色素浓缩激素受体拮抗剂，用作中枢疾病、循环系统疾病和代谢疾病的药物。 [解决方法] 提供了一种日萘基甲酰胺衍生物，其表示为式（I）：其中，R1a、R1b、R2a、R2b、R3a和R3b独立地表示氢原子或类似物，R4表示氢原子、C1-6烷基或类似物，R5表示氢原子或类似物，Z表示C1-6烷基或类似物，或者R4和Z共同形成一个含有氮的4-6元杂环，Y1表示H或类似物，Y2表示H，或者Y1和Y2共同形成-O-CH2-，W表示C、SO或类似物，Ar1表示6元芳基或类似物，Ar2表示6元芳基或类似物，环A表示苯环、吡啶环或类似物。